1. Field of the Invention
The present invention involves a pharmaceutical formulation which permits injection of an amino-steroid drug without hemolysis.
2. Description of the Related Art
16.alpha.-Methyl-21-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]-1-piperaziny l]pregna-1,4,9(11)-triene-3,20-dione is known as the free base, the monomethanesulfonate, dimethanesulfonate or hydrochloride salts, see International Publication No. W087/01706.
Cancer Chemotherapy Reports Part I, 58, 171 (1974) and J. Pharm. Exptl. Ther., 196, 525 (1976) report that ellipticine (an antineoplastic agent active against L1210 lymphocytic leukemia) causes hemolysis and hypotension in dogs and monkeys following intravenous injection. The hemolysis was prevented when ellipticine was prepared in 300 milliosmoles citrate buffer, pH=4.0. Even though hemolysis was prevented, ellipticine still produced hypotension, bradycardia and an increase in carotid artery blood flow.
The pharmaceutical formulation of the present invention not only prevents hemolysis but it also prevents hypotension.
A presentation of the composition of the present invention was made on Dec. 7, 1987 at Poster Session N-4 (N 07-W-02) of the Pharmaceutics and Pharmaceutical Technology section of the Japanese-United States Congress of Pharmaceutical Sciences' meeting.